Ligands-for-Target-Protein-for-PROTAC-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html Ligands HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html for HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK h

2、ttps:/www.MedChemE/Targets/Ligand for Target Protein.html Target HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html Protein HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www

3、.MedChemE/Targets/Ligand for Target Protein.html for HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html PROTACTarget Protein-binding MoietyThe PROTAC molecule consists of a target protein ligand and an E3 ubiquiti

4、n ligase ligand, with a linker binds them together. Theligand for target protein will lead to attachment of a PROTAC to the proteins of interest for ubiquitin and subsequent degradation.Target proteins are usually proteins whose overexpression or accumulation may play important roles in the progress

5、 of diseases.Numbers of PROTACs have been developed to degrade kinases (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (suchas p53, STAT, RAR, ER and AR), epigenetic tools (such as HDAC and BET bromodomain) and E3 ligase themselves (such as MDM2).www.MedChemE 1 HYPERLINK https:/www.MedCh

6、emE/Targets/Ligand for Target Protein.html Ligands HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html for HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/

7、Ligand for Target Protein.html Target HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html Protein HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand fo

8、r Target Protein.html for HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html PROTAC HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Prot

9、ein.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html & HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html HYPERLINK https:/www.MedChemE/Targets/Ligand for Target Protein.html Ch

10、emicals HYPERLINK https:/www.MedChemE/_addition_-JQ-1.html (+)-JQ-1(JQ1) Cat. No.: HY-13030 HYPERLINK https:/www.MedChemE/a-1210477-piperazinyl.html A-1210477-piperazinyl(PROTAC Mcl1-binding moiety 1) Cat. No.: HY-125908(+)-JQ-1 (JQ1) is a potent, specific, andreversible BET bromodomain inhibitor, w

11、ithIC s of 77 and 33 nM for the first and second50bromodomain (BRD4(1/2). (+)-JQ-1 also activatesautophagy.A-1210477-piperazinyl is a compound binds toprotein myeloid cell leukemia 1 (MCL1) used forPROTAC technology.Purity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10

12、 mg, 50 mg, 100 mg, 200 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac.html Abemaciclib HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac.html HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac.html metabolite HYPERLINK http

13、s:/www.MedChemE/cdk-ligand-for-protac.html HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac.html M18(LSN3106729) Cat. No.: HY-126534 HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac-hydrochloride.html Abemaciclib HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac-hydrochloride.html HYPERLINK

14、https:/www.MedChemE/cdk-ligand-for-protac-hydrochloride.html metabolite HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac-hydrochloride.html HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac-hydrochloride.html M18 HYPERLINK https:/www.MedChemE/cdk-ligand-for-protac-hydrochloride.html HYPERLINK h

15、ttps:/www.MedChemE/cdk-ligand-for-protac-hydrochloride.html hydrochloride(LSN3106729 hydrochloride) Cat. No.: HY-126534AAbemaciclib metabolite M18 (LSN3106729), themetabolite of Abemaciclib (HY-16297A), is a CDKinhibitor with antitumor activity. Abemaciclibmetabolite M18 and a CRBN ligand have been

16、used todesign PROTAC CDK4/6 degrader.Abemaciclib metabolite M18 (LSN3106729)hydrochloride, the metabolite of Abemaciclib(HY-16297A), is a CDK inhibitor with antitumoractivity. Abemaciclib metabolite M18 hydrochlorideand a CRBN ligand have been used to design PROTACCDK4/6 degrader.Purity: 98%Clinical

17、 Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.01%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/abemaciclib-metabolite-m18-d8.html Abemaciclib HYPERLINK https:/www.MedChemE/abemaciclib-metabolite-m18-d8.html HYPERLIN

18、K https:/www.MedChemE/abemaciclib-metabolite-m18-d8.html metabolite HYPERLINK https:/www.MedChemE/abemaciclib-metabolite-m18-d8.html HYPERLINK https:/www.MedChemE/abemaciclib-metabolite-m18-d8.html M18-d8(LSN3106729-d8) Cat. No.: HY-126534S HYPERLINK https:/www.MedChemE/abm-14.html ABM-14Cat. No.: H

19、Y-131388Abemaciclib metabolite M18-d8 (LSN3106729-d8) isthe deuterium labeled Abemaciclib metabolite M18.Abemaciclib metabolite M18 (LSN3106729), themetabolite of Abemaciclib (HY-16297A), is a CDKinhibitor with antitumor activity.ABM-14 is a ligand for targeting androgenreceptor (AR) for PROTAC. ABM

20、-14 binds to aligand for VHL via linker to form ARCC-4(HY-130492) to degrade AR.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/androgen-receptor-antagonist-1.html

21、Androgen HYPERLINK https:/www.MedChemE/androgen-receptor-antagonist-1.html HYPERLINK https:/www.MedChemE/androgen-receptor-antagonist-1.html receptor HYPERLINK https:/www.MedChemE/androgen-receptor-antagonist-1.html HYPERLINK https:/www.MedChemE/androgen-receptor-antagonist-1.html antagonist HYPERLI

22、NK https:/www.MedChemE/androgen-receptor-antagonist-1.html HYPERLINK https:/www.MedChemE/androgen-receptor-antagonist-1.html 1 HYPERLINK https:/www.MedChemE/androgen-receptor-antagonist-1.html HYPERLINK https:/www.MedChemE/androstanolone-acetate.html Androstanolone HYPERLINK https:/www.MedChemE/andr

23、ostanolone-acetate.html HYPERLINK https:/www.MedChemE/androstanolone-acetate.html acetateCat. No.: HY-130992(Dihydrotestosterone acetate) Cat. No.: HY-111847Androgen receptor antagonist 1 is an orallyavailable full androgen receptor (AR)antagonist with an IC of 59 nM.50Androstanolone acetate is an a

24、ndrogen ligand,which targets androgen receptor (AR).Androstanolone acetate binds to cIAP1 ligandBestatin via a linker to form PROTACs.Purity: 99.39%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 2

25、5 mg HYPERLINK https:/www.MedChemE/protac-fkbp12-ligand-1.html AP1867-2-(carboxymethoxy) HYPERLINK https:/www.MedChemE/protac-fkbp12-ligand-1.html HYPERLINK https:/www.MedChemE/ap1867-3-methoxyethylamine.html AP1867-3-(aminoethoxy)(PROTAC FKBP12-binding moiety 2) Cat. No.: HY-114420Cat. No.: HY-1293

26、63AP1867-2-(carboxymethoxy), the AP1867 (a syntheticFKBP12F36V-directed ligand) based moiety, binds toCRBN ligand via a linker to form dTAG molecules.AP1867-3-(aminoethoxy), the AP1867 based moiety,is a synthetic ligand for FKBP.AP1867-3-(aminoethoxy) can be used in thesynthesis of PROTAC FKBP12 F36

27、V degrader.Purity: 96.44%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/apcin-

28、a.html Apcin-ACat. No.: HY-130841 HYPERLINK https:/www.MedChemE/crabp-ii-ligand-1.html ATRA-hydroxyimino(CRABP-II ligand 1) Cat. No.: HY-111839Apcin-A, an Apcin derivative, is ananaphase-promoting complex (APC) inhibitor.Apcin-A interacts strongly with Cdc20, andinhibits the ubiquitination of Cdc20

29、substrates.Apcin-A can be used to synthesize the PROTAC CP5V(HY-130257).ATRA-hydroxyimino (CRABP-II ligand 1), theRetinoic acid (ATRA)-based moiety, binds to cIAP1ligand (Bestatin) via a linker to form SNIPER todegrade CRABP-II in IMR-32 cells.Purity: 98.0%Clinical Data: No Development ReportedSize:

30、 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bet-in-6.html BET-IN-6 HYPERLINK https:/www.MedChemE/bet-in-6.html HYPERLINK https:/www.MedChemE/bi-4464.html BI-4464Cat. No.: HY-130813 Cat. No.: HY-124625BE

31、T-IN-6 is a potent and high affnity BRD2/BRD4inhibitor. BET-IN-6 is the ligand for targetprotein BRD2/4, and is used for the systhesis ofPROTAC BRD2/BRD4 degrader-1 (HY-130612).BI-4464 is a highly selective ATP competitiveinhibitor of PTK2/FAK, with an IC of 17 nM. A50PTK2 ligand for PROTAC.Purity:

32、98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.27%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bms-1166-n-piperidine-cooh.html BMS-1166-N-piperidine-COOH HYPERLINK https:/www.MedChemE/bms-1166-n-piperidine-cooh.html HYPERLI

33、NK https:/www.MedChemE/cbp-p300-ligand-2.html CBP/p300 HYPERLINK https:/www.MedChemE/cbp-p300-ligand-2.html HYPERLINK https:/www.MedChemE/cbp-p300-ligand-2.html ligand HYPERLINK https:/www.MedChemE/cbp-p300-ligand-2.html HYPERLINK https:/www.MedChemE/cbp-p300-ligand-2.html 2Cat. No.: HY-131187 Cat.

34、No.: HY-138539BMS-1166-N-piperidine-COOH, the BMS-1166-basedmoiety, binds to E3 ligase ligand via a linker toform PROTAC PD-1/PD-L1 degrader-1 (HY-131183) todegrade PD-1/PD-L1. BMS-1166 is a potentPD-1/PD-L1 interaction inhibitor with an IC of501.4 nM.CBP/p300 ligand 2 is a ligand for target protein

35、for PROTAC of dCBP-1. dCBP-1 is a potent andselective heterobifunctional degrader of p300/CBP.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK http

36、s:/www.MedChemE/ccr7-ligand-1.html CCR7 HYPERLINK https:/www.MedChemE/ccr7-ligand-1.html HYPERLINK https:/www.MedChemE/ccr7-ligand-1.html Ligand HYPERLINK https:/www.MedChemE/ccr7-ligand-1.html HYPERLINK https:/www.MedChemE/ccr7-ligand-1.html 1 HYPERLINK https:/www.MedChemE/ccr7-ligand-1.html HYPERL

37、INK https:/www.MedChemE/cdk9-in-10.html CDK9-IN-10(CCR7-Cmp2105) Cat. No.: HY-133073Cat. No.: HY-130850CCR7 Ligand 1 (CCR7-Cmp2105) is an allostericLigand and antagonist for human CC chemokinereceptor 7 (CCR7) with a K of 3 nM. CCR7dLigand 1, thiadiazole-dioxide ligan, suppressesarrestin binding in

38、response to activation byCCL19 with an IC of 7.3 M.50Purity: 99.64%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mgCDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10is the ligand for the PROTAC CDK9 degrader-2(HY-112811).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

39、HYPERLINK https:/www.MedChemE/cdk9-in-11.html CDK9-IN-11 HYPERLINK https:/www.MedChemE/cdk9-in-11.html HYPERLINK https:/www.MedChemE/rar-ligand-1.html Ch55-O-C3-NH2Cat. No.: HY-130852(RAR ligand 1) Cat. No.: HY-111843CDK9-IN-11 is a potent CDK9 inhibitor. CDK9-IN-11is the ligand for the PROTAC CDK9

40、Degrader-1(HY-103628).Ch55-O-C3-NH2 (RAR ligand 1) is a Ch 55-basedligand, which targets RAR. Ch55-O-C3-NH2 (RARligand 1) binds to cIAP1 ligand Bestatin via alinker to form SNIPER.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize:

41、1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-4.html Dasatinib HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-4.html HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-4.html carbaldehyde(BMS-354825 carbaldehyde; PROTAC ABL binding moiety 4) Cat. No.:

42、 HY-111857 HYPERLINK https:/www.MedChemE/protac-brd4-binding-moiety-4-1.html Desmethyl-QCA276(PROTAC BRD4-binding moiety 4) Cat. No.: HY-44103Dasatinib carbaldehyde (BMS-354825 carbaldehyde),the Dasatinib (ABL inhibitor) based moiety, bindsto IAP ligand via a linker to form SNIPER .Desmethyl-QCA276

43、(PROTAC BRD4-binding moiety 4),the QCA276-based moiety, binds to cereblon ligandvia a linker to form PROTAC to degrade BET.QCA276 is a BET inhibitor with an IC of 10 nM,50and with a K of 2.3 nM.iPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development

44、 ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/desmorpholinyl-navitoclax-nh-me.html Desmorpholinyl HYPERLINK https:/www.MedChemE/desmorpholinyl-navitoclax-nh-me.html HYPERLINK https:/www.MedChemE/desmorpholinyl-navitoclax-nh-me.html Navitoclax-NH-Me(Desmorpholinyl ABT-263-NH-Me) Cat. No.: H

45、Y-131232 HYPERLINK https:/www.MedChemE/dimethyl-f-oicr-9429-cooh.html Dimethyl-F-OICR-9429-COOHCat. No.: HY-141799Desmorpholinyl Navitoclax-NH-Me is a Bcl-xLinhibitor. Desmorpholinyl Navitoclax-NH-Me and aCRBN ligand for the E3 ubiquitin ligase can beused in the synthesis of PROTAC BCL-XL degraderXZ

46、739 (HY-133557).Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeatdomain protein 5 (WDR5) extracted from patentWO2019246570A1 intermediate 19.Dimethyl-F-OICR-9429-COOH can be used in thesynthesis of PROTACs.Purity: 99.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100

47、 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/dupa.html DUPA HYPERLINK https:/www.MedChemE/dupa.html HYPERLINK https:/www.MedChemE/eed226-cooh.html EED226-COOHCat. No.: HY-111606 Cat. No.: HY-130979DUPA, belongs to a class of glutamate ureas, isus

48、ed as the targeting moiety in drug conjugate toselectively deliver cytotoxic drugs to prostatecancer cells.EED226-COOH is an EED226-derived ligand for targetprotein EED ligand for PROTAC, binds to a ligandfor VHL via linker to form UNC6852 (HY-130708) todegrade PRC2.Purity: 98.0%Clinical Data: No De

49、velopment ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/er-alpha-ligand-1.html Estrone-N-O-C1-amido HYPERLINK https:/www.MedChemE/er-alpha-ligand-1.html HYPERLINK https:/www.MedC

50、hemE/fn-1501-propionic-acid.html FN-1501-propionic HYPERLINK https:/www.MedChemE/fn-1501-propionic-acid.html HYPERLINK https:/www.MedChemE/fn-1501-propionic-acid.html acid(ER ligand 1) Cat. No.: HY-111845Cat. No.: HY-130981Estrone-N-O-C1-amido (ER ligand 1) is anEstrone-based estrogen ligand, which

51、targetsestrogen receptor (ER). Estrone-N-O-C1-amido(ER ligand 1) binds to cIAP1 ligand Bestatin via alinker to form SNIPER.FN-1501-propionic acid is a CDK2/9 ligand forPROTAC. FN-1501-propionic acid and a CRBN ligandhave been used to design PROTAC CDK2/9 degrader(HY-130709).Purity: 98%Clinical Data:

52、 No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-2.html GNF5-amido-Me HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-2.html HYPERLINK https:/www.MedChemE/protac-abl-binding-moiet

53、y-3.html HG-7-85-01-Decyclopropane(PROTAC ABL binding moiety 2) Cat. No.: HY-111852 (PROTAC ABL binding moiety 3) Cat. No.: HY-111855GNF5-amido-Me, the GNF5 (ABL inhibitor) basedmoiety, binds to IAP ligand via a linker to formSNIPER.HG-7-85-01-Decyclopropane, the HG-7-85-01 (ABLinhibitor) based moie

54、ty, binds to IAP ligand via alinker to form SNIPER .Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Target_Protein-binding_moiety

55、_4.html I-BET762 HYPERLINK https:/www.MedChemE/Target_Protein-binding_moiety_4.html HYPERLINK https:/www.MedChemE/Target_Protein-binding_moiety_4.html carboxylic HYPERLINK https:/www.MedChemE/Target_Protein-binding_moiety_4.html HYPERLINK https:/www.MedChemE/Target_Protein-binding_moiety_4.html acid

56、 HYPERLINK https:/www.MedChemE/Target_Protein-binding_moiety_4.html (Molibresib carboxylic acid;GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2)Cat. No.: HY-107443 HYPERLINK https:/www.MedChemE/PCI-32765.html Ibrutinib(PCI-32765) Cat. No.: HY-10997I-BET762 carboxylic acid (Molibresib carbox

57、ylicacid) is an I-BET762-based warhead ligand forconjugation reactions of PROTAC targeting on BET.I-BET762 carboxylic acid (Molibresib carboxylicacid) is a BRD4 inhibitor with a pIC of 5.1.50Ibrutinib (PCI-32765) is a selective, irreversibleBtk inhibitor with an IC of 0.5 nM.50Purity: 98.64%Clinical

58、 Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mgPurity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-1.html Imatinib HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-1.h

59、tml HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-1.html carbaldehyde HYPERLINK https:/www.MedChemE/protac-abl-binding-moiety-1.html (CGP-57148B carbaldehyde; STI571carbaldehyde; PROTAC ABL binding moiety 1) Cat. No.: HY-111849 HYPERLINK https:/www.MedChemE/ipatasertib-nh2.html Ipatasertib

60、-NH2(GDC-0068-NH2; RG7440-NH2) Cat. No.: HY-130988Imatinib carbaldehyde (CGP-57148B carbaldehyde),the Imatinib (ABL inhibitor) based moiety, bindsto IAP ligand via a linker to form SNIPER.Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is aligand for target protein AKT for PROTAC(INY-03-041). INY-03-041 i